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PLA/PLGA shell-core microballoons prepared by oil in water-solid in oil method, and preparation method thereof

A solid-in-oil and oil-in-water technology, which is applied in the preparation of shell-core microspheres and its preparation, can solve the problems of incomplete release and inability to overcome the encapsulation rate, and achieve good redispersibility

Inactive Publication Date: 2009-06-24
SHANGHAI JIAO TONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But still can not overcome the low encapsulation efficiency, there are shortcoming of sudden release and incomplete release

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Example 1: Preparation of PLA / PLGA shell-core microspheres loaded with small molecule drug particles

[0031] (1) Prepare small molecule drugs or small molecule drugs and pharmaceutical excipients into drug granules;

[0032] In this embodiment, the small molecule drugs used are tumor chemotherapy drugs (tumor chemotherapy drugs are selected from: doxorubicin, cyclophosphamide, dactinomycin, bleomycin, daunorubicin, doxorubicin, epirubicin Mitomycin, Mitomycin, Methotrexate, Fluorouracil, Carboplatin, Carmustine (BCNU), Semustine, Cisplatin, Etoposide, Camptothecin and its derivatives, Cholesterol , paclitaxel and its derivatives, docetaxel and its derivatives, vinblastine, vincristine, tamoxifen, etoposide, piposulfan, cyclophosphamide, or flutamide and its derivatives; sustained release Microspheres can be loaded with one or more of the above drugs;) or antibiotics (antibiotics are selected from cyclosporine, levofloxacin, ofloxacin, or epinastine hydrochloride; slow...

Embodiment 2

[0047] Example 2: Preparation of PLA / PLGA shell-core microspheres loaded with biomacromolecular drug particles

[0048] (1) Prepare biomacromolecular drugs or biomacromolecular drugs and pharmaceutical excipients into drug granules;

[0049] In this example, the biomacromolecular drugs used are erythropoietin (EPO), recombinant human granulocyte colony-stimulating factor (G-CSF), granulocyte-macrophage colony-stimulating factor (GM-CSF), vaccines, Interferon (INF), growth hormone (GH), insulin (Insulin), epidermal growth factor (EGF), fibroblast growth factor (FGF), transforming growth factor (TGF-β), insulin-like growth factor (IGF), Vascular endothelial growth factor (VEGF), platelet growth factor (PDGF), endothelial growth factor (ECGF), nerve growth factor (NGF), bone-derived growth factor (BDGF), bone morphogenic protein (BMP), tissue polypeptide antigen ( TPA), antibody (antibody), coagulation factor VIII (VIII), genetic factor IX, antisense nucleotide (anti-RNA), small...

Embodiment 3

[0062] Embodiment three: the preparation of loading interferon (IFN) drug particle PLA / PLGA shell-core microsphere

[0063] (1) Prepare interferon and pharmaceutical excipients into pharmaceutical granules; the specific ratio is as follows:

[0064] drug

medical supplements

Drug accounted for particle weight

volume percentage drug

medical supplements

Drug accounted for particle weight

volume percentage IFN

Dextran

80%, 50%, 25%

%, 10% or 5%

IFN

Cyclodextrin and sucrose (9:1),

(7:1), (6:1), (5:1)

or (3:1) 100%, 80%, 50%

%, 25% or 10%

IFN

Dextran, zinc salts and

Trehalose (9:1:1)

80%, 50%, 25%

%, 10% or 5%

IFN

polyethylene glycol, chitosan and

Sorbitol (8:1:1) or

(5:1:1) 100%, 80%, 50%

%, 25% or 10%

IFN

Glucan and Seaweed

Sugar (9:1)

80%, 50%, 25%

%, 10% or 5%

IFN

Dextran, Glycine and Glycine

Dew...

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PUM

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Abstract

The invention relates to a PLA / PLGA shell-core microsphere prepared by solid-in-oil-in-water in the technical field of pharmacy and a preparation method thereof. The microsphere comprises 0.01 to 50 percent of medicine, 20 to 99.99 percent of polylactic acid and / or polylactic acid-glycolic acid, or / and 0 to 30 percent of pharmaceutical excipient (weight percentage). The method comprises the steps of: adding medicine particles into a PLA and / or PLGA organic solution to be emulsified, then selecting a hydrophilic organic solvent to re-emulsify to form unhardened balls, finally hardening in another large oil phase, removing the organic solvent and collecting micropheres. The method overcomes the disadvantages of low envelope rate of the prior W / O and W / O / W, serious burst release of S / O / O, and environmental pollution, controls the grain diameter of the microsphere according to the need, does not pollute the environment, and can be applied to the preparation of slow release or controlled release microspheres of various medicines and adjuvants of vaccines.

Description

technical field [0001] The present invention relates to preparation of shell-core microspheres and its preparation method in the field of pharmaceutical technology, especially a method for preparing PLA (polylactic acid) / PLGA (polylactic acid-glycolic acid) from oil-in-water-solid-in-oil (S-O-W) ) shell-core microsphere method. Background technique [0002] In the pharmaceutical industry, from drug discovery to clinical application, the last link is drug preparation. Some of the drugs need long-term administration to be cured; others need targeted and other local administration. To achieve these goals, raw materials must be prepared into corresponding dosage forms. For example, drugs that require long-term administration but have a short half-life in the body should be prepared into PLA dosage forms; for the treatment of some tumors, some drugs need to be targeted to the disease, such as embolization microsphere preparations that target tumor blood vessels; gene recombinat...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K47/34
Inventor 金拓袁伟恩吴飞赵昊任甜甜
Owner SHANGHAI JIAO TONG UNIV
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